Letrozole

Cytostatic · Non-steroidal aromatase inhibitor

Indications

Advanced post-menopausal breast-cancer resistant to tamoxifen or other anti-oestrogens.

Dosage

Adults: 1 tab daily. Children: Not applicable.

Adverse Effects

Musculoskeletal pain, headache, GI upset, dyspnoea, cough, chest pain, viral infections, hot flushes, abdominal pain, fatigue, hypercholesterolaemia, sweating, appetite changes, depression, dizziness, palpitations, hypertension, alopecia, rash, dry skin, arthralgia, myalgia, bone pain, osteoporosis, arthritis, vaginal bleeding, peripheral oedema, wt changes. Reports of cardiovascular events.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Positive evidence of risk: Use only when no safer alternative exists for a serious problem. Lactation: Contraindicated or not recommended. Contraindications: Pre-menopausal women, very severe hepatic impairment, pre-op use if receptor status negative or unknown. Precautions: Monitor bone mineral density during adjuvant therapy in women with or at risk of osteoporosis. Very severe renal impairment, severe hepatic impairment.

Interactions

Tamoxifen, oestrogens. Substrates of CYP2A6 or CYP2C19 that have a narrow therapeutic index.

Advice to Patient

Take with or without meals. Consult prescriber for mild analgesic if you have musculoskeletal pain or headache. Contact prescriber if there is skin rash, severe nausea, muscle pain, difficulty in breathing, chest pain, palpitations, swelling of extremities, weakness, numbness, severe headache, difficulty in speaking, unusual signs of bruising or bleeding, vaginal bleeding, difficulty in breathing.

Pharmacokinetics

Absorption: Rapid and well absorbed; not affected by food. Metabolism: Hepatic. Half-life elimination: Terminal: Approx. 2 days. Time to steady state, plasma: 2 to 6 weeks; steady state serum concentrations are 1.5 to 2 times higher than single-dose values. In girls 3 to 9 years, steady state concentrations were 25% to 67% that of the mean adult values. Excretion: Urine.

Brands with this active ingredient

Compiled by Healify Pharmacy from published drug references. How we compile it →

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